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双氟沙星对兔源金黄色葡萄球菌分离株的处置动力学、药代动力学及药代动力学-药效学整合

Disposition kinetics and pharmacokinetics--pharmacodynamic integration of difloxacin against Staphylococcus aureus isolates from rabbits.

作者信息

Fernández-varón E, Cárceles C M, Marín P, Vancraeynest D, Montes A, Sotillo J, García-Martínez J D

机构信息

Department of Pharmacology, Faculty of Veterinary Medicine, University of Murcia, Murcia, Spain.

出版信息

Res Vet Sci. 2008 Feb;84(1):90-4. doi: 10.1016/j.rvsc.2007.04.002. Epub 2007 Jun 15.

DOI:10.1016/j.rvsc.2007.04.002
PMID:17573085
Abstract

The pharmacokinetics of difloxacin were studied following intravenous (IV), subcutaneous (SC) and oral administration of 5mg/kg to healthy white New Zealand rabbits (n = 6). Difloxacin concentrations were determined by HPLC assay with fluorescence detection. Minimal inhibitory concentrations (MICs) assay of difloxacin against different strains of S. aureus from different european countries was performed in order to compute the main pharmacodynamic surrogate markers. The plasma difloxacin clearance (Cl) for the IV route was (mean +/- SD) 0.41 +/- 0.05 L/h kg. The steady-state volume of distribution (V(ss)) was 1.95 +/- 0.17 L/kg. The terminal half-life [Formula: see text] was (mean+/-SD) 4.19+/-0.34 h, 7.53 +/- 1.32 h and 8.00 +/- 0.45 h after IV, IM and oral, respectively. From this data, it seems that a 5 mg/kg dose difloxacin would be effective by SC and oral routes in rabbits against bacterial isolates with MIC0.1 microg/mL.

摘要

对健康的白色新西兰兔(n = 6)静脉注射(IV)、皮下注射(SC)和口服5mg/kg的二氟沙星后,研究了其二氟沙星的药代动力学。通过带有荧光检测的高效液相色谱法(HPLC)测定二氟沙星浓度。为了计算主要的药效学替代指标,对来自不同欧洲国家的不同金黄色葡萄球菌菌株进行了二氟沙星的最低抑菌浓度(MICs)测定。静脉注射途径的血浆二氟沙星清除率(Cl)为(平均值±标准差)0.41±0.05 L/h·kg。稳态分布容积(V(ss))为1.95±0.17 L/kg。静脉注射、肌肉注射和口服后,终末半衰期[公式:见原文]分别为(平均值±标准差)4.19±0.34小时、7.53±1.32小时和8.00±0.45小时。根据这些数据,5mg/kg剂量的二氟沙星通过皮下和口服途径对MIC为0.1μg/mL的兔细菌分离株似乎有效。

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